T 0978/02 (Pyrrolopyrimidines/NOVARTIS) of 10.5.2006

Summary of Facts and Submissions

I. This appeal lies from the decision of the Examining Division refusing the present European patent application 97 940 108.0 (published under number WO 98/07726), which relates to substituted pyrrolopyrimidines and processes for their preparation.

II. The application in suit was refused on the ground that the subject-matter of Claim 1, corresponding to pages 62 and 63 as originally filed and page 64 filed on 25 July 2001, lacked novelty and inventive step in view of documents:

(1) WO 95/19774, and

(2) EP-A-0 682 027.

III. Said Claim 1 forming the basis of the decision under appeal read as follows:

"A 7H-pyrrolo[2,3-d]pyrimidine derivative of the formula I

FORMULA/TABLE/GRAPHIC

in which n is 0 to 3,

q is 0 or 1,

R is halogen, lower alkyl, hydroxymethyl, aminomethyl, hydroxyl, lower alkanoyloxy, lower alkoxy, carboxyl, lower alkanoyl, benzoyl, lower alkoxycarbonyl, carbamoyl, N-lower alkylcarbamoyl, N,N-di-lower alkylcarbamoyl, cyano, amino, lower alkanoylamino, lower alkylamino, N,N-di-lower alkylamino or trifluoromethyl, it being possible, if two or more radicals R are present in the molecule, for these to be identical to or different from one another,

one of the radicals R1 and R2 is hydrogen or lower alkyl,

and the other of the radicals R1 and R2 is

a) a radical of the formula II

FORMULA/TABLE/GRAPHIC

in which u is 1 to 3 and

at least one radical R4 is amidino, guanidino, ureido, N**(3)-lower alkylureido, N**(3),N**(3)-di-lower alkylureido, N**(3)-phenylureido, N**(3),N**(3)-diphenylureido, thiocarbamoyl, thioureido, N**(3)-lower alkylthioureido, N**(3),N**(3)-di-lower alkylthioureido, lower alkoxycarbonylamino, benzyloxycarbonylamino, morpholine-4-carbonyl, piperazine-1-carbonyl, 4-lower alkylpiperazine-1-carbonyl, lower alkylsulfonylamino, benzenesulfonylamino, toluenesulfonylamino, thiophene-2-carbonylamino, furan-2-carbonylamino, benzylamino, hydroxymethyl, aminomethyl or a radical of the formula -N=C(R5)-R6, in which R5 is hydrogen or lower alkyl and R6 is di-lower alkylamino, piperidino, 4-lower alkylpiperazino or morpholino, and the other radical(s) R4 is(are) halogen, lower alkyl, hydroxyl, lower alkanoyloxy, lower alkoxy, carboxyl, lower alkoxycarbonyl, carbamoyl, N-lower alkylcarbamoyl, N,N-di-lower alkylcarbamoyl, cyano, amino, lower alkanoylamino, lower alkylamino, N,N-di-lower alkylamino or trifluoromethyl, it being possible, if two or more radicals R4 are present in the molecule, for these to be identical to or different from one another, or is

b) a radical of the formula III

FORMULA/TABLE/GRAPHIC

in which R7 is lower alkoxy or benzyloxy and R8 is hydroxyl or benzyloxy, or is

c) amino-lower alkyl, whose amino group is substituted by one or two hydroxy-lower alkyl, amino-lower alkyl, carboxy-lower alkyl, lower alkoxycarbonyl-lower alkyl, benzyloxycarbonyl-lower alkyl or benzyl radicals, which in the phenyl moiety are unsubstituted or substituted by halogen, lower alkyl, hydroxymethyl, aminomethyl, hydroxyl, lower alkanoyloxy, lower alkoxy, carboxyl, lower alkanoyl, benzoyl, lower alkoxycarbonyl, carbamoyl, N-lower alkylcarbamoyl, N,N-di-lower alkylcarbamoyl, cyano, amino, lower alkanoylamino, lower alkylamino, N,N-di-lower alkylamino or trifluoromethyl, or is

d) piperidine-1-carbonyl, piperazine-1-carbonyl, 4-lower alkylpiperazine-1-carbonyl, morpholine-4-carbonyl, thiocarbamoyl, a heterocyclic radical bonded via a ring carbon atom and having five ring members and 1-4 ring heteroatoms, selected from oxygen, nitrogen and sulfur, or is

e) 4-lower alkylpiperazinomethyl or a lower alkyl radical which is substituted by a heterocyclic radical other than piperazinyl and having five or six ring members and 1-4 ring heteroatoms, selected from oxygen, nitrogen and sulfur, or is

f) a radical of the formula -CH=N-OR9 in which R9 is hydrogen or lower alkyl, or

g) if q is 1, additionally to the definitions given above in the sections a) to f) can also be phenyl which is substituted by halogen, lower alkyl, trifluoromethyl or lower alkoxy, and

R3 is hydrogen, lower alkyl, lower alkoxycarbonyl, carbamoyl, N-lower alkylcarbamoyl or N,N-di-lower alkylcarbamoyl,

or its salts,

wherein the prefix "lower" denotes a radical having up to and including a maximum 0f 7 carbon atoms."

IV. Concerning the issue of inventive step the Examining Division held in particular

- that, like the present application, both documents (1) and (2) related to 7H-pyrrolo[2,3-d]pyrimidine derivatives having an anti-tumour activity,

- that document (1) disclosed a group of compounds having an overlap with the group of compounds as claimed in Claim 1 of the application in suit and containing a bridging group corresponding to the group -(HR3)q- as defined in Claim 1 of the application in suit in which q is 0 or 1, thus teaching that this bridging group might be present or not, and

- that it would be obvious to the skilled person in the light of document (2) that effective pyrrolo[2,3-d]pyrimidine derivatives could have substituents in the 6-position as defined in D(2) for R2 and claimed in Claim 1 of the present application as indicated under g).

V. Oral proceedings before the Board were held on 10 May 2006.

VI. The Appellant defended the patentability of the subject-matter of the present application on the basis of Claims 1 to 7 submitted during these oral proceedings as its sole request.

Claim 1 of this request read as follows:

"A 7H-pyrrolo[2,3-d]pyrimidine derivative of the formula I

FORMULA/TABLE/GRAPHIC

in which n is 0 or 1,

q is 0 or 1,

R is chlorine,

R1 is hydrogen,

R2 is

a) a radical of the formula II

FORMULA/TABLE/GRAPHIC

in which u is 1 and

R4 is N**(3)-lower alkylureido, N**(3)-phenylureido, N**(3)-lower alkylthioureido, lower alkoxycarbonylamino, benzyloxycarbonylamino, morpholine-4-carbonyl, piperazine-1-carbonyl, 4-lower alkylpiperazine-1-carbonyl, lower alkylsulfonylamino, benzenesulfonylamino, toluenesulfonylamino, furan-2-carbonylamino, thiophene-2-carbonylamino, benzylamino, hydroxymethyl or a radical of the formula -N=C(R5)-R6, in which R5 is hydrogen or lower alkyl and R6 is di-lower alkylamino, piperidino, 4-lower alkylpiperazino or morpholino, or is

b) a radical of the formula III

FORMULA/TABLE/GRAPHIC

in which R7 is lower alkoxy and R8 is hydroxyl or benzyloxy, or is

c) piperazine-1-carbonyl, 4-lower alkylpiperazine-1-carbonyl, morpholine-4-carbonyl, thiocarbamoyl, thiazol-2-yl, 4-(4-methoxyphenyl)thiazole-2-yl, 4,5-dimethylthiazol-2-yl, tetrazol-5-yl, 2-methyltetrazol-5-yl, 1-methyltetrazol-5-yl, or is

d) a radical of the formula -CH=N-OR9 in which R9 is hydrogen or lower alkyl, and

R3 is hydrogen, lower alkyl,

or a pharmaceutical acceptable salt thereof,

wherein the prefix "lower" denotes a radical having up to and including a maximum 0f 7 carbon atoms."

With respect to the subject-matter of this Claim 1 the appellant argued in particular that, by restricting the subject-matter of the former Claim 1, the overlap of the claimed group of compounds with the group of compounds disclosed in document (1) had been removed. Moreover, it argued with respect to the question of inventive step that neither document (1) nor document (2) provided an incentive to the provision of effective 7H-pyrrolo[2,3-d]pyrimidine derivatives having in the 6-position a substituent as defined in present Claim 1 for R2.

VII. The Appellant requested that the decision under appeal be set aside, and that a patent be granted on the basis of Claim 1 of the request filed during the oral proceedings.

VIII. At the conclusion of the oral proceedings the Board´s decision was pronounced.

Reasons for the Decision

1. The appeal is admissible.

2. Amendments (Article 123(2) EPC)

Present Claim 1 is supported by Claim 3 of the application as filed in combination with the description as filed, page 3, second paragraph, with respect to the prefix "lower".

2.1 Therefore, the Board concludes that the subject-matter of Claim 1 of the present request does not extend beyond the content of the application as filed, and consequently meets the requirement of Article 123(2) EPC.

3. Novelty

3.1 Neither document (1) nor document (2) discloses a 7H-pyrrolo[2,3-d]pyrimidine derivative having in the 6-position a substituent as defined in present Claim 1 for R2.

3.2 Consequently, the Board concludes that the claimed subject-matter is novel.

4. Inventive step and remittal

4.1 Although the Board considers, in agreement with the Appellant, that the cited documents (1) and (2) alone or in combination do not suggest the provision of 7H-pyrrolo[2,3-d]pyrimidine derivatives falling under the scope of the strongly restricted subject-matter of present Claim 1, that subject-matter has not been examined by the first instance with respect to the essential issue of inventive step. Moreover, the Examining Division did not decide the question of the patentability of the further dependent and independent claims then on file, let alone the further and restricted claims filed during the oral proceedings before the Board.

4.2 Under these circumstances the Board considers it appropriate to exercise its power conferred on it by Article 111(1) EPC to remit the case to the Examining Division for further prosecution on the basis of Claim 1 filed during the oral proceedings.

ORDER

For these reasons it is decided that:

1. The decision under appeal is set aside.

2. The case is remitted to the first instance for further prosecution on the basis of Claim 1 of the sole request filed during the oral proceedings.